title: [Identification of the functional activity of synthetic polyamine analogues using a biotest system based on highly proliferating cultured human cells].
abstract: A new biotest system was developed based on highly proliferating human cell cultures (lines LNCaP and PC-3). With the help of this system, two known synthetic polyamines--alpha-difluoromethylornithine (DFMO) and methylglioxalbis(guanylhydrason) (MGBG)--as well as four new synthetic analogues difenyl containing amines (DFCA-1-DFCA-4) with molecular weights of 725.5 (DFCA-1), 755.5 (DFCA-2), 655.5 (DFCA-3), and 681.5 Da (DFCA-4) were tested. In this biotest system, DFMO (0.1-400 microM) did not reveal functional activity, whereas for MGBG a cytotoxic effect was registered (100-200 microM). DFCA-1, DFCA-2, and DFCA-4 had a similar effect at concentrations of 10 microM and higher; DFCA-3, at a concentration of 50 microM and higher. Thus, DFCA-1 has a higher level of antiproliferating activity and may be considered as the most potent cytostatic agent.
authors.forename: K V
authors.initials: KV
authors.lastname: Lisitskaia
authors.forename: N A
authors.initials: NA
authors.lastname: Sokueva
authors.forename: Iu G
authors.initials: IuG
authors.lastname: Malysheva
authors.forename: A V
authors.initials: AV
authors.lastname: Ivanov
authors.forename: S S
authors.initials: SS
authors.lastname: Shishkin
authors.forename: S P
authors.initials: SP
authors.lastname: Siatkin
mesh_terms: D001681:Biological Assay; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D054697:Cytostatic Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D000518:Eflornithine / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D008297:Male; D008935:Mitoguazone / Q000138:chemical synthesis / Q000494:pharmacology*; D011073:Polyamines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D001713:Biphenyl Compounds; D054697:Cytostatic Agents; D011073:Polyamines; D008935:Mitoguazone; D000518:Eflornithine